|
Market Research Report
|
Day 1 | Day 2 | Short Courses | Download Brochure
MONDAY, NOVEMBER 2 7:00 am Registration and Morning Coffee
KEYNOTE SESSION 8:30 Chairperson’s Opening Remarks
Gregory J. Kaczorowski, Ph.D., Adjunct Professor, Physiology and Pharmacology, New Jersey Medical School; Adjunct Professor, Physiology and Biophysics, Robert Wood Johnson Medical School Ion channels are important targets of therapeutic agents. Historically, it has been challenging to develop drugs on this target class. A major issue with target based ion channel drug development is identification of good small molecule chemical leads for Medicinal Chemistry optimization to clinical candidate status. Recently, many unique strategies have been developed for ultra high throughput screening of ion channel targets to identify tractable chemical leads in large sample collections. These efforts have been successful in identifying novel modulators of voltage-dependent sodium, calcium and potassium channels. A number of case histories addressing the design and implementation of these novel approaches will be presented.
Michael Dabrowski, Ph.D., Head, Global Ion Channel Initiative, AstraZeneca R&D In 2007, AstraZeneca launched an internal Global Ion Channel Initiative with the aim to fill the gaps in ion channel lead generation. We recruited 9 postdoctoral fellows in electrophysiology, chemistry and molecular cell biology and invested in relevant technologies focusing on ion channel lead generation: e.g. new ion channel targeted chemical libraries, new and better assay formats on existing technology platforms and cutting edge gene delivery and expression systems. In my talk I will show results obtained by the postdoc team improving ion channel lead generation capabilities and also discuss the use of postdocs in this Big Pharma initiative.
David Clapham, M.D., Ph.D., Aldo R. Castañeda Professor of Cardio-vascular Research, Investigator, Howard Hughes Medical Institute
10:10 Grand Opening Coffee Break in the Exhibit Hall Structural Studies 10:40 Expression and Purification of Human TRPV1 for Structural Studies Alla Korepanova, Ph.D., Department of Structural Biology, GPRD, Abbott Laboratories High-yield heterologous protein production has been a major limiting step in structural characterization of membrane proteins including ion channels. TRPV1 is a ligand-gated ion channel that is involved in acute thermal nociception and neurogenic inflammation. Full-length human TRPV1 was expressed in HIfgh-Five insect cells using the baculovirus expression system. Efficient solubilization and purification procedures resulted in milligram amounts of detergent-solubilized channel at 80 -90% purity. Protein functionality was confirmed by ligand binding. Developed methods can be applied to other TRPV1and mammalian ion channels. 11:10 Structural Insights into the Function of TRPV Channels Rachelle Gaudet, Ph.D., Associate Professor, Department of Molecular and Cellular Biology, Harvard University This presentation will describe insights into the function of TRPV channels gained through crystallography, biochemistry and electrophysiology. In particular, the cytoplasmic ankyrin repeats of thermosensitive TRPV channels regulate the sensitivity of TRPV channel responses to multiple stimuli. Both nucleotides and calmodulin interact with the ankyrin repeats and mediate the channel response to changes in cytoplasmic calcium levels.
Sponsored by Mark Slack, Ph.D., Senior Scientist, Cellular Assays, Evotec, AG Numerous clinical projects have been delayed or stopped due to safety pharmacologically issues associated with the hERG ion channel. Anti-histamines have a history of such negative effects on hERG and thus in the development and optimization of potent Histamine receptor 3 (H3) antagonists. Is was desirable to address these liabilities early in the chemical optimization. Within the medicinal chemistry optimization of key H3 scaffolds, carefully selected compounds were analyzed in electrophysiological measurements for their apparent hERG inhibition. The resulting 3D computational model supported the medicinal chemistry to optimize affinity to the H3 target while avoiding hERG liability. In the presentation, the benefits of the approach for the lead series will be shown. 12:10 pm Hits Validation Using Endogenous Ion Channels Expressed on Human CD4+ T Cells Melisa Ho, Ph.D., Senior Research Scientist, Wyeth Research 12:40 Luncheon Presentation (Sponsorship Opportunity Available) or Lunch on Your Own
2:20 Chairperson’s Remarks
2:25 Cardiovascular Arrhythmia Safety in Drug Development, Inhibition of the Late Ina Current to Stabilize Ventricular Repolarization, and Late Ina as a Therapeutic Target Philip Sager, M.D., Vice President, Clinical Research, Gilead Sciences, Inc. Luiz Belardinelli, Ph.D., Senior Vice President, Pharmacology and Translational Biomedical Research, CV Therapeutics, Inc. There have been major advances in the evaluation of cardiac safety during drug development and the understanding of ionic mechanisms to destabilize and stabilize ventricular repolarization. This 2 part presentation will cover the major aspects of CV arrhythmia evaluation during drug development, the impact of preclinical data on the early clinical trials, and new research findings, focusing on the Late Ina current, to stabilize ventricular repolarization. Recent data has shown that inhibition of Late Ina can prevent arrhythmogenesis, even in the setting of administration of an arrhythmogenic drug such as one that inhibits hERG. In addition, therapeutic implications of modifying the Late Ina current will be discussed.
3:25 Title to be Announced Derek J. Trezise, Ph.D., Director, Biological Reagents & Assay Development, GlaxoSmithKline 3:55 Networking Refreshment Break in the Exhibit Hall 4:30 Calcium Channelopathies in Neurological Diseases Philippe Lory, Ph.D., Institut de Génomique Fonctionnelle, Département de Physiologie, CNRS Childhood absence epilepsy, familial hemiplegic migraine, episodic ataxia type 2 and autism spectrum disorder are rare inherited forms of common neurological disorders. The genetic basis of these calcium channelopathies provides unique opportunities to study the underlying mechanisms from the molecular to organism levels. Studies of channelopathies illuminate relationships between channel structure and function, and reveal diverse and unexpected physiological roles for these channels. Importantly, these studies also lead to screening for drugs to prevent acquired channel disorders, as well as to novel therapeutic practices. 5:00 Sponsored Presentation (Opportunity Available) 5:15 Ion Channels in Metabolic Diseases Chuan-Chu Chou, Ph.D., Research Fellow, Schering Plough Research Institute Ion channels play dominant roles under many pathophysiological conditions, including cardiovascular disorder, pain, and respiratory diseases. Despite the fact of over $6 billion in sales per year the market for ion-channel modulators remains under-exploited. Diabetes represents one of the largest global therapeutic demands and a top challenge to the pharmaceutical industry. This presentation will focus on ion channels as an emerging class of therapeutic targets for diabetes. Several lines of promising experimental evidence and their relevance to the disease in humans will be discussed. 5:45 Happy Hour in the Exhibit Hall 7:00 Close of Day Day 1 | Day 2 | Short Courses | Download Brochure Suggested Event Package (November 1 – 4): November 1 Pre-Conference Short Courses: Targeting GPCRs and Ion Channels with Antibodies (SC2) AND Structure-Based Design of Ion Channels (SC5) November 2 - 3 Conference: Ion Channels as Therapeutic Targets – A Flood of Potential for Drug Discovery November 3 - 4 Conference: Kinase Inhibitors: Moving from Discovery to Development OR Targeting Diabetes with Novel Therapeutics: Advancing Clinical Candidates
|
   
.jpg "AppliedBiosystems")  .jpg "Gloucester Pharma")    .jpg "Biovex-Neurovex"){kind=small} .jpg "PQ")  .jpg "taconic resized 170") |
||
|
|
||||
.jpg "Accuri")
